Table 1

Competitive inhibitors of human microsomal tolbutamide 4′-hydroxylation and diclofenac 4′-hydroxylation (CYP2C9)

InhibitorKi(apparent)1-a
μM
LY2138293.5  ± 0.4
LY1567351-b 4.4  ± 0.9
LY3005021-b 8.0  ± 0.4
LY3359791-b 12.3  ± 3.0
Piroxicam16.9  ± 2.6
Phenytoin1-c 17.1  ± 1.5
Clozapine1-c 31.1  ± 2.2
LY30016433.8  ± 1.6
LY3335311-b 94.3  ± 14.2

The inhibitor constant was determined as described underExperimental Procedures.

  • 1-a  Parameter estimate ± S.E. of the parameter estimate.

  • 1-b  Diclofenac 4′-hydroxylation.

  • 1-c  Ring et al., 1996.